1305124-48-4Relevant academic research and scientific papers
The involvement of the mitochondrial amidoxime reducing component (MARC) in the reductive metabolism of hydroxamic acidsS
Ginsel, Carsten,Plitzko, Birte,Froriep, Danilo,Stolfa, Diana A.,Jung, Manfred,Kubitza, Christian,Scheidig, Axel J.,Havemeyer, Antje,Clement, Bernd
, p. 1396 - 1402 (2018)
The mitochondrial amidoxime reducing component is a recently discovered molybdenum enzyme in mammals which, in concert with the electron transport proteins cytochrome b5 and NADH cytochrome b5 reductase, catalyzes the reduction of N-oxygenated structures.
Efficient new constructs against triple negative breast cancer cells: Synthesis and preliminary biological study of ferrocifen-SAHA hybrids and related species
Cazares Marinero, Jose De Jesus,Lapierre, Marion,Cavailles, Vincent,Saint-Fort, Renette,Vessieres, Anne,Top, Siden,Jaouen, Gerard
, p. 15489 - 15501 (2013/11/06)
Chemotherapeutic agents combining several active groups within a single molecule can modulate multiple cellular pathways and, thus, exhibit higher efficacy than single-target drugs. In this study, six new hybrid compounds combining tamoxifen (TAM) or ferrocifen (FcTAM) structural motifs with suberoylanilide hydroxamic acid (SAHA) were synthesised and evaluated. Antiproliferative activity was first explored in cancer cell lines. Combining FcTAM and SAHA structural motifs to form the unprecedented FcTAM-SAHA hybrid molecule led to an increased cytotoxicity (IC50 = 0.7 μM) in triple-negative MDA-MB-231 breast cancer cells when compared to FcTAM or SAHA alone (IC50 = 2.6 μM and 3.6 μM, respectively), while the organic hybrid analogue TAM-SAHA was far less cytotoxic (IC50 = 8.6 μM). In hormone-dependent MCF-7 breast cancer cells, FcTAM-SAHA was more active (IC50 = 2.0 μM) than FcTAM (IC50 = 4.4 μM) and TAM-SAHA (IC50 > 10 μM), but less toxic than SAHA (IC 50 = 1.0 μM). Surprisingly, FcTAM-PSA, an N1- phenylsuberamide derivative, also possessed strong antiproliferative activity (IC50 = 0.5 μM and 1.8 μM in MDA-MB-231 and MCF-7 cells, respectively). Subsequent biochemical studies indicate that estrogen receptor alpha (ERα) and histone deacetylases (HDAC) are not the main targets of the hybrid compounds for their antiproliferative effect. Interestingly, both organometallic compounds were able to induce p21waf1/cip1 gene expression in MCF-7 breast cancer cells in accordance with their antiproliferative activity.
COMPOUNDS AND METHODS
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Page/Page column 32, (2013/05/22)
The present invention relates to compounds that inhibit histone deacetylase (HDAC) enzymes, the preparation of these compounds or salts of said compound, the use of these compounds in the treatment of neurodegenerative diseases or conditions ameliorated by inhibition of HDAC activity and pharmaceutical compositions that are comprised of these compounds.
